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. 2011 Jan 1;21(1):288-93.
doi: 10.1016/j.bmcl.2010.11.015. Epub 2010 Nov 5.

Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases

Michel Gallant  1 , Christian Beaulieu, Carl Berthelette, John Colucci, Michael A Crackower, Chad Dalton, Danielle Denis, Yves Ducharme, Richard W Friesen, Daniel Guay, François G Gervais, Martine Hamel, Robert Houle, Connie M Krawczyk, Birgit Kosjek, Stephen Lau, Yves Leblanc, Ernest E Lee, Jean-François Levesque, Christophe Mellon, Carmela Molinaro, Wayne Mullet, Gary P O'Neill, Paul O'Shea, Nicole Sawyer, Susan Sillaots, Daniel Simard, Deborah Slipetz, Rino Stocco, Dan Sørensen, Vouy Linh Truong, Elizabeth Wong, Jin Wu, Helmi Zaghdane, Zhaoyin Wang
Affiliations

Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases

Michel Gallant et al. Bioorg Med Chem Lett. .

Abstract

In this manuscript we wish to report the discovery of MK-7246 (4), a potent and selective CRTH2 (DP2) antagonist. SAR studies leading to MK-7246 along with two synthetic sequences enabling the preparation of this novel class of CRTH2 antagonist are reported. Finally, the pharmacokinetic and metabolic profile of MK-7246 is disclosed.

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